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Interaction of the anti-tuberculous drug bedaquiline with artificial membranes and rat erythrocytes
Chemico-Biological Interactions ( IF 4.7 ) Pub Date : 2018-11-26 , DOI: 10.1016/j.cbi.2018.11.017
Konstantin N. Belosludtsev , Nikita V. Penkov , Kirill S. Tenkov , Eugeny Yu. Talanov , Natalia V. Belosludtseva , Alexey V. Agafonov , Anastasia E. Stepanova , Vlada S. Starinets , Olga V. Vashchenko , Sergey V. Gudkov , Mikhail V. Dubinin

Bedaquiline (BDQ) is a new drug from the family of diarylquinolines, which has a potent bactericidal activity against Mycobacterium tuberculosis. This paper has examined the interaction of BDQ with model membranes (liposomes and BLM) and rat erythrocytes. It was shown that BDQ (1–10 mol%) changed the thermotropic phase behavior of DMPC liposomes, leading to the lateral phase separation in the lipid bilayer and the formation of membrane microdomains. BDQ (10–50 μM) was also demonstrated to cause permeabilization of lecithin liposomes loaded with the fluorescent dye sulforhodamine B. At the same time, it did not alter the ionic conductivity of BLM. A dynamic light scattering study showed that BDQ led to the emergence of two populations of light-scattering particles in the suspension of lecithin liposomes, suggesting that an aggregation of the vesicles took place. In rat erythrocytes, BDQ was found to induce changes in their size and shape, as well as aggregation and lysis of the cells.



中文翻译:

抗结核药物苯达喹啉与人造膜和大鼠红细胞的相互作用

Bedaquiline(BDQ)是二芳基喹啉家族的新药,对结核分枝杆菌具有有效的杀菌活性。本文研究了BDQ与模型膜(脂质体和BLM)和大鼠红细胞的相互作用。结果表明,BDQ(1-10 mol%)改变了DMPC脂质体的热致相行为,导致脂质双层中的侧向相分离和膜微区的形成。BDQ(10–50μM)也被证明可导致卵磷脂脂质体中的荧光染料磺基若丹明B透化。同时,它不会改变BLM的离子电导率。一项动态光散射研究表明,BDQ导致卵磷脂脂质体悬浮液中出现了两个群体的光散射颗粒,这表明囊泡发生了聚集。在大鼠红细胞中,发现BDQ诱导其大小和形状以及细胞聚集和裂解的变化。

更新日期:2018-11-26
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